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New methodologies to synthetise unnatural nucleosides, known and putative antiproliferative agents

Final Activity Report Summary - MEDCHEM AT QUB/GSK (New methodologies to synthetise unnatural nucleosides, known and putative antiproliferative agents)

MEDCHEM at QUB/GSK aimed at providing a structure for scientists in the early stage of their career wanting to acquire high quality experience and training in the pharmaceutical industry while pursuing an innovative and academically challenging PhD programme.

The research training carried out at Queen's University Belfast (QUB) and at GlaxoSmithKline (GSK) offered an opportunity to most early stage researchers (ESRs) enrolled on this program, who were 10 in total over the four project years, to acquire a fully integrated academic and industrial training specialised in research areas of medicinal, biological and synthetic chemistry.

All researchers enrolled on this programme had first-hand access to industrial perspective to their project as well as on site experience. While each researcher pursued individual research, the overall perspective of the programme was to establish novel methodologies to access c-glycosides and c-nucleosides as putative antiviral or antibacterial agents. In order to address this we developed complementary synthetic methods to prepare novel and structurally diverse c-nucleoside and c-glycoside scaffolds. The explored chemical strategies involved chemoenzymatic processes, multi-step one pot syntheses and use of renewable resources, in addition to the development of novel advanced synthetic methodologies and extensive analytical protocols.

In addition to carrying out traditional carbon based chemistry, phosphorus based chemistry was extensively pursued, particularly in relation to the preparation of sugar and nucleoside diphosphate analogues such as nicotinamide adenine dinucleotide, adenosine diphosphate ribose and mannose diphosphate guanosine.